AT-9283 was being developed by Astex Pharmaceuticals as a treatment for cancer and myelofibrosis. AT-9283 is an inhibitor of mitosis (cell division) and is the second most progressed drug candidate in the Astex portfolio of novel molecularly targeted cancer drugs. All of Astex’s current products have been discovered internally using its proprietary drug discovery approach. AT9283 is a potent inhibitor of the Aurora A and B kinases and has been shown to arrest tumour growth in a range of tumour models. Aurora kinases play a key role in mitotic checkpoint control in cell division. Both Aurora A and B are over-expressed in many human tumours and are believed to be excellent targets for anti-cancer therapy.

DS-3032 (Milademetan) is an orally available, potent and selective inhibitor of the p53-MDM2 (murine double minute 2) interaction. Milademetan binds to, and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. Milademetan is 10-fold more potent than the first-generation inhibitor nutlin-3a. By preventing this MDM2-p53 interaction, the proteasome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored. This results in the restoration of p53 signaling and leads to the p53-mediated induction of tumor cell apoptosis. DS-3032 is currently being evaluated in three phase 1 clinical trials for solid and hematological malignancies, including acute myeloid leukemia (AML), acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML) in blast phase, lymphoma and myelodysplastic syndrome (MDS).

GNF-156 (ganaplacide or KAF-156) is an antimalarial agent that is part of the imidazolopiperazine family. It exerts activity against pre-erythrocytic liver stages, asexual and sexual blood stages. An improvement compared to existing antimalarial drug combinations is that this compound shows promising single-dose antimalarial activity, and no serious safety and tolerability concerns in humans are known so far. Phase II clinical trials have been completed for GNF-156. Its potential is also being investigated in combination with lumefantrine (an aryl-amino alcohol) in LUM-KAF156.

(+)-Epicatechin or ent-Epicatechin is one of the 4 catechin diastereoisomers. (+)-Epicatechin has been isolated from various species of Palmae. It is occurred in the leaves or fruit of six palm species. In addition, it was isolated from Dryas octopetala and guarana seeds. It resists to the microbial transformation by endophytic fungi isolated from a tea plant.

F2BMET (redaporfin or LUZ11), a fluorinated sulfonamide bacteriochlorin, is photosensitizer, with antineoplastic activity upon photodynamic therapy. F2BMET is a third generation bacteriochlorin molecule which has a greater ability to absorb light and convert it into active molecular species (reactive oxygen species), better depth penetration, and improved efficacy. F2BMET has promising Phase I/IIA POC clinical data in advanced head and neck cancer which clearly reinforces the favorable results from non-clinical studies. It has received Orphan Drug Designation (ODD) from EMA in Europe for Biliary tract cancer.